AAI101
(Synonyms: Enmetazobactam) 目录号 : GC32165A β-lactamase inhibitor
Cas No.:1001404-83-6
Sample solution is provided at 25 µL, 10mM.
Enmetazobactam is a β-lactamase inhibitor.1 It has greater activity against class A β-lactamases (IC50s = 0.006-0.52 ?M) than class B or class D β-lactamases (IC50s = 8.7->100 ?M). Enmetazobactam in combination with the cephalosporin antibiotic cefepime is active against 223 Enterobacteriaceae clinical isolates, including multidrug-resistant E. coli and K. pneumoniae isolates, with an MIC50 value of 0.125 mg/L.2 In vivo, enmetazobactam reduces mortality in mouse models of septicemia induced by E. coli, K. pneumoniae, or E. cloacae when used in combination with cefepime.1
1.Papp-Wallace, K.M., Bethel, C.R., Caillon, J., et al.Beyond piperacillin-tazobactam: Cefepime and AAI101 as a potent β-lactam-β-lactamase inhibitor combinationAntimicrob Agents Chemother.63(5)e00105-00119(2019) 2.Crandon, J.L., and Nicolau, D.P.In vitro activity of cefepime/AAI101 and comparators against cefepime non-susceptible EnterobacteriaceaePathogens4(3)620-625(2015)
Animal experiment: |
The 20 Enterobacteriaceae strains are used to infect groups of three mice each. At 2 h after inoculation, mice are treated with humanized regimens of cefepime or cefepime-AAI101. All doses are administered as 0.2-mL subcutaneous injections. To serve as control animals, an additional group of mice is administered normal saline at the same volume and frequency and by the same route. Thighs from all animals are harvested at 24 h after initiation of therapy. The harvesting procedure for all study mice began with euthanasia by CO2 exposure, followed by cervical dislocation. After sacrifice, thighs are removed and homogenized individually in normal saline. For determinations of the numbers of CFU, serial dilutions of thigh homogenates are spread onto Trypticase soy agar with 5% sheep blood using a spiral plater. In addition to the aforementioned treatment and control groups, another group of three infected but untreated mice is harvested at the initiation of dosing and served as a 0-h control. Efficacy, expressed as the change in bacterial density, is determined by calculation of the change in the log10 number of CFU obtained in mice after 24 h of treatment from the densities observed in the 0-h control animals. |
References: [1]. Crandon JL, et al. In Vitro Activity of Cefepime/AAI101 and Comparators against Cefepime Non-susceptible Enterobacteriaceae. Pathogens. 2015 Aug 18;4(3):620-5. |
Cas No. | 1001404-83-6 | SDF | |
别名 | Enmetazobactam | ||
Canonical SMILES | C[N+]1=NN(C[C@@](S([C@]2([H])C3)(=O)=O)(C)[C@H](C([O-])=O)N2C3=O)C=C1 | ||
分子式 | C11H14N4O5S | 分子量 | 314.32 |
溶解度 | DMSO : ≥ 113.3 mg/mL (360.46 mM) | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1815 mL | 15.9074 mL | 31.8147 mL |
5 mM | 0.6363 mL | 3.1815 mL | 6.3629 mL |
10 mM | 0.3181 mL | 1.5907 mL | 3.1815 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet